Desmopressin Acetate (DDAVP), a synthetic peptide analog of vasopressin, is a safe antidiuretic and hemostatic compound that acts as a selective agonist at the vasopressin V2 membrane receptor (V2R)[1].
Desmopressin Acetate has moderate antiproliferative activity, and at low cell densities Desmopressin Acetate significantly inhibited F3II cell colony formation with an IC50 value of 700 nM. Conditioned media from F3II monolayers exposed to low doses of Desmopressin Acetate (100 nM) significantly increased angiostatin formation in the presence of purified plasminogen. Following heterologous V2R expression, Desmopressin Acetate induces cyclic adenosine monophosphate (cAMP)-dependent endothelial nitric oxide synthase (eNOS) activation via Ser1177 phosphorylation[2].
Co-injection of Desmopressin Acetate (1-2 μg/kg) at the time of i.v. injection of F3II or LM3 cells significantly inhibited the formation of tumor lung metastases in a mouse lung metastasis model of breast cancer, with a reduction of approximately 70% in the number of lung nodules in both cases[3]. Dogs undergoing surgery for intervertebral disc disease had a significantly prolonged buccal mucosal bleeding time (BMBT) after aspirin administration, but preoperative intravenous administration of Desmopressin Acetate rapidly reversed the prolongation of the BMBT, and none of them experienced intraoperative bleeding complications[4].
References:
[1] Ripoll G V, Garona J, Pifano M, et al. Reduction of tumor angiogenesis induced by desmopressin in a breast cancer model[J]. Breast cancer research and treatment, 2013, 142: 9-18.
[2] Kaufmann J E, Iezzi M, Vischer U M. Desmopressin (DDAVP) induces NO production in human endothelial cells via V2 receptor-and cAMP-mediated signaling[J]. Journal of Thrombosis and Haemostasis, 2003, 1(4): 821-828.
[3] Alonso D F, Skilton G, Farías E F, et al. Antimetastatic effect of desmopressin in a mouse mammary tumor model[J]. Breast cancer research and treatment, 1999, 57: 271-275.
[4] Di Mauro F M, Holowaychuk M K. Intravenous administration of desmopressin acetate to reverse acetylsalicylic acid‐induced coagulopathy in three dogs[J]. Journal of Veterinary Emergency and Critical Care, 2013, 23(4): 455-458.
Desmopressin Acetate（DDAVP）是加压素的合成肽类似物，是一种安全的抗利尿和止血化合物，可作为血管加压素V2膜受体（V2R）的选择性激动剂[1]。
Desmopressin Acetate具有适度的抗增殖活性，在低细胞密度时Desmopressin Acetate可显著抑制F3II细胞集落形成，IC50值为700 nM。在纯化纤溶酶原存在的情况下，F3II单层细胞暴露于低剂量Desmopressin Acetate（100 nM）的条件培养基中会显著增加血管生成素的形成[1]。在异源V2R表达后，Desmopressin Acetate可通过Ser1177磷酸化诱导环磷酸腺苷（cAMP）依赖性内皮一氧化氮合酶（eNOS）激活[2]。
在静脉注射F3II或LM3细胞时共注射Desmopressin Acetate（1-2 μg/kg）显著抑制乳腺癌小鼠肺转移模型中肿瘤肺转移的形成，肺结节数量均减少约70%[3]。接受椎间盘疾病手术的狗在服用阿司匹林后颊粘膜出血时间（BMBT）明显延长，但术前静脉给予Desmopressin Acetate迅速逆转了BMBT的延长，并且均未出现术中出血并发症[4]。